Yang Chang, Bai Jie, Du Shou-Ying, Cui Ya-Hua, Zhang Qin-Shuai, Ma Jun-Ming
Beijing University of Chinese Medicine, Beijing 100102, China.
Zhongguo Zhong Yao Za Zhi. 2016 Nov;41(22):4247-4253. doi: 10.4268/cjcmm20162226.
To establish a method for detecting micro-dialysis recovery of paeonol, eugenol and piperine in Huoxue Zhitong patch, in order to provide the basis for further percutaneous pharmacokinetics studies. The concentrations of paeonol, eugenol and piperine in dialysates were determined by HPLC, and probe deliveries were calculated respectively. The effects of concentration and calibration approaches on the micro-dialysis probe deliveries of the three components were investigated, and their probe absorbability, in vitro and in vivo probe stability and repeatability were also studied.The results indicated that little paeonol, eugenol and piperine were observed in probes with 30% alcohol as the perfusate, and could be cleaned from probe in a short time. And the in vivo and in vitro probe deliveries of three components were stable within 8 h, drug-containing solution and blank perfusate were alternatively used for three times, and the in vivo and in vitro probe deliveries of three components were basically unchanged. The in vitro recoveries of paeonol, eugenol and piperine with a range of concentration were respectively (45.7±4.66)%, (27.82±2.95)%, (41.3±3.96)%, which indicated no concentration independent. Under the same conditions, the similar delivery was observed by dialysis, retrodialysis and no-net flux. Therefore, the concentrations of analyses of the collected fraction could be calibrated by in vitro or in vivo recoveries. Meanwhile, this also proved that the micro-dialysis method built by this study is applicable to the study on percutaneous pharmacokinetics of Huoxue Zhitong patch.
建立一种检测活血止痛贴中丹皮酚、丁香酚和胡椒碱微透析回收率的方法,为进一步开展经皮药代动力学研究提供依据。采用高效液相色谱法测定透析液中丹皮酚、丁香酚和胡椒碱的浓度,并分别计算探针回收率。考察浓度和校准方法对三种成分微透析探针回收率的影响,同时研究其探针吸附性、体内外探针稳定性及重复性。结果表明,以30%乙醇为灌注液时,探针中丹皮酚、丁香酚和胡椒碱含量极少,且能在短时间内被清除。三种成分的体内外探针回收率在8 h内稳定,含药溶液和空白灌注液交替使用3次,三种成分的体内外探针回收率基本不变。不同浓度的丹皮酚、丁香酚和胡椒碱体外回收率分别为(45.7±4.66)%、(27.82±2.95)%、(41.3±3.96)%,表明回收率与浓度无关。在相同条件下,透析法、反透析法和无净通量法的回收率相近。因此,收集组分的分析浓度可通过体外或体内回收率进行校准。同时,这也证明了本研究建立的微透析方法适用于活血止痛贴经皮药代动力学研究。